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Updated: Jun 22, 2025

Synthesis of Wavelength-shifting DNA Hybridization Probes by Using Photostable Cyanine Dyes
Published on: July 6, 2016
Isothiocyanate intermediates facilitate divergent synthesis of N-heterocycles for DNA-encoded libraries
Huihong Wang1,2, Teng Chen2, Xiaohong Fan1
1Pharmaceutical Department, Chongqing University Three Gorges Hospital, Chongqing University, 404100 Chongqing, P. R. China. delight9924@163.com.
Abstract:
The versatile reactivity of isothiocyanate intermediates enabled the diversity-oriented synthesis (DOS) of N-heterocycles in a DNA-compatible manner. We first reported a mild in situ conversion of DNA-conjugated amines to isothiocyanates. Subsequently, a set of diverse transformations was successfully developed to construct 2-thioxo-quinazolinones, 1,2,4-thiadiazoles, and 2-imino thiazolines. Finally, the feasibility of these approaches in constructing DELs was further demonstrated through enzymatic ligation and mock pool preparation. This study demonstrated the advantages of combining in situ conversion strategies with DOS, which effectively broadened the chemical and structural diversity of DELs.
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